Delving into the Latest Updates on Imrecoxib with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Erechrome, 恒扬

Target

COX-2

Mechanism

COX-2 inhibitors(Cyclooxygenase-2 inhibitors)

Therapeutic Areas

Immune System DiseasesSkin and Musculoskeletal Diseases

Active Indication

Osteoarthritis

Inactive Indication

Acute PainOsteoarthritis, KneeRenal Insufficiency

Originator Organization

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Active Organization

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Inactive Organization

Institute of Materia Medica

Drug Highest PhaseApproved

First Approval Date

CN (20 May 2011),

Osteoarthritis

RegulationSpecial Review Project (CN)

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Structure

Molecular FormulaC21H23NO3S

InChIKeyAXMZZGKKZDJGAZ-UHFFFAOYSA-N

CAS Registry395683-14-4

INTRODUCTIONNonsteroidal anti-inflammatory drugs (NSAIDs) are the primary treatment for osteoarthritis (OA), but prolonged use has adverse effects and varying efficacy. Among NSAIDs, imrecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, reduces side effects yet remains ineffective for half of the patient population. This study aims to identify biomarkers for early evaluation of imrecoxib efficacy in OA for personalized therapy optimization.METHODSFrom September 2021 to January 2022, imrecoxib was administered to patients with OA at Nanjing Drum Tower Hospital. Plasma samples from these patients underwent proteomic analysis through the four-dimensional data-independent acquisition (4D-DIA) method, followed by bioinformatics analysis. Potential differentially expressed proteins (DEPs) were validated using enzyme-linked immunosorbent assays (ELISA).RESULTSSixty-six patients with knee OA were included and divided into responders (n = 35) and non-responders (n = 31). Proteomic analysis was conducted on 15 patients from each group, with ELISA validation for every patient. We found 140 DEPs between the two groups after imrecoxib treatment, characterized by 29 proteins showing upregulation and 111 displaying downregulation (P < 0.05, fold change > ± 1.2). Galectin-1 (LGALS1), galectin-3 (LGALS3), and cluster of differentiation 44 (CD44) were identified as potential markers for evaluating clinical response to imrecoxib in OA following ELISA validation.CONCLUSIONThis study successfully identified biomarkers for evaluating imrecoxib's clinical response in patients with OA using 4D-DIA technology. These biomarkers may play a vital role in future personalized OA treatment strategies, pending further confirmation.

01 Nov 2023·Heliyon

Imrecoxib attenuates bleomycin-induced pulmonary fibrosis in mice

Article

Author: Meng, Lingxin ; Zhang, Yanping ; Li, Xiaohe ; Gao, Jingjing ; Zhang, Jianwei ; Miao, Yang ; Yang, Yue ; Mao, Jiahe ; Gu, Xiaoting ; Yang, Cheng ; Zhou, Honggang

Idiopathic pulmonary fibrosis (IPF) is an incurable chronic progressive disease with a low survival rate and ineffective therapeutic options. We examined the effects of imrecoxib, a nonsteroidal anti-inflammatory drug, on experimental pulmonary fibrosis. The mouse IPF model was established by intratracheal instillation of bleomycin. From Day 0 to Day 13, the mice were orally administered imrecoxib (100 mg/kg) and pirfenidone (200 mg/kg) daily, and from Day 7 to Day 13, the mice were orally administered pirfenidone and imrecoxib daily. The tissues were dissected on the 14th day. Mouse body weight was measured, and histopathological examination and hydroxyproline content analysis confirmed that the administration of imrecoxib exerted a similar effect to pirfenidone. Compared with bleomycin-induced mice, imrecoxib-treated mice showed significantly reduced inflammatory factor expression (IL-1 and TNF-α) and inflammatory cell numbers (macrophages, lymphocytes, and neutrophils) in BALF (bronchoalveolar lavage fluid). Our experiment tested the ability of imrecoxib to inhibit the signal pathway involved in gene expression induced by TGF-β1 in the NIH-3T3 cell line in vitro. Western blotting showed that imrecoxib (20 μM and 40 μM) inhibited the expression of fibronectin, type I collagen and CTGF. In addition, imrecoxib reduced the levels of p-ERK1/2. The changes in the expression of related proteins in mouse lung tissue were similar to those in cells. In summary, our findings suggested that the administration of imrecoxib prevented and treated murine IPF by inhibiting inflammation and the TGF-β1-ERK1/2 signaling pathway.

12 Aug 2023·Zhongguo zhen jiu = Chinese acupuncture & moxibustion

[Evaluation of the clinical effect of acupuncture in treatment of neck pain in cervical spondylosis based on propensity score matching].

Article

Author: Yang, Zhi-Xin ; Guo, Jian-En ; Wang, Yu-Man ; Zhang, Yin-Juan ; Yang, Jia-Qi ; Wu, Jie ; Liu, Jin-Ying

OBJECTIVETo observe the clinical effect and safety of acupuncture in treatment of neck pain due to cervical spondylosis.METHODSAccording to the patients' preference and acceptance for the interventions of neck pain induced by cervical spondylosis, an acupuncture group (221 cases) and a non-acupuncture group (251 cases) were divided. After the control of confounding factors with propensity score matching, 218 cases were included in either acupuncture group or non-acupuncture group. In the acupuncture group, acupuncture was applied to Dazhui (GV 14), Baihui (GV 20), ashi points, bilateral neck-Jiaji (EX-B 2), Fengchi (GB 20), Houxi (SI 3), Shenmai (BL 62), etc. The treatment was given once daily, one course of intervention was composed of 5 treatments and 3 courses were included. In the non-acupuncture group, the oral administration of imrecoxib tablets and cobalt tablets was prescribed for 2 weeks. Before and after treatment, the scores of Northwick Park questionnaire (NPQ) and the simplified McGill pain questionnaire (SF-MPQ) were observed, and the safety was assessed in patients of the two groups.RESULTSAfter treatment completion, the scores of NPQ and SF-MPQ were all reduced when compared with those before treatment in each group (P<0.001), and the scores of NPQ and SF-MPQ in the acupuncture group were lower than those of the non-acupuncture group (P<0.001). The incidence of adverse reactions was 6.0% (13/218) in the acupuncture group and was 10.1% (22/218) in the non-acupuncture group, without statistical significance in comparison (P>0.05).CONCLUSIONAcupuncture is effective and safe in the relief of neck pain and the improvement of comprehensive quality of life in the patients with cervical spondylosis.

100 Deals associated with Imrecoxib

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	M01AH	DB12354

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Osteoarthritis	CN	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	20 May 2011

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Acute Pain	Phase 1	CN	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	19 Dec 2018

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


EULAR2017	Not Applicable	Axial Spondyloarthritis VEGF \| BMP-2 \| COX-2 ... View more	120	Imrecoxib	brirgsycpz(ogsihokdeg) = wcyuqipdpc kvhoqdnsog (bljpordkip ) View more	-	14 Jun 2017
				Celecoxib	brirgsycpz(ogsihokdeg) = sfaaogjyed kvhoqdnsog (bljpordkip ) View more